Matryoshka-type gastro-resistant microparticles for the oral treatment of Mycobacterium tuberculosis

Aim: Production of Matryoshka-type gastroresistant microparticles containing antibiotic-loaded poly lactic-co-glycolic acid (PLGA) nanoparticles (NP) against Mycobacterium tuberculosis. Materials & methods: The emulsification and evaporation methods were followed for the synthesis of PLGA-NPs and methacrylic acid-ethyl acrylate-based coatings to protect rifampicin from degradation under simulated gastric conditions. Results & conclusion: The inner antibiotic-loaded NPs here reported can be released under simulated intestinal conditions whereas their coating protects them from degradation under simulated gastric conditions. The encapsulation does not hinder the antituberculosis action of the encapsulated antibiotic rifampicin. A sustained antibiotic release could be obtained when using the drug-loaded encapsulated NPs. Compared with the administration of the free drug, a more effective elimination of M. tuberculosis was observed when applying the NPs against infected macrophages. The antibiotic-loaded PLGA-NPs were also able to cross an in vitro model of intestinal barrier. Matryoshka-type gastroresistant microparticles containing antibiotic-loaded poly lactic-co-glycolic acid nanoparticles against M. tuberculosis were produced to protect the antibiotic from degradation under simulated gastric conditions. The antibiotic-loaded poly lactic-co-glycolic acid nanoparticles were able to cross an in vitro model of intestinal barrier, being more effective in the elimination of M. tuberculosis when applied against infected macrophages compared with the use of the free drug. </inline-graphic.